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1. 发明授权

US08790619B2 Indole derivatives 有权
标题翻译：吲哚衍生物
公开(公告)号：US08790619B2
公开(公告)日：2014-07-29
申请号：US13258465
申请日：2010-03-26
申请人： Harry John Wadsworth , Bo Shan , Dennis O'Shea , Joanna Marie Passmore , William John Trigg , Amanda Ewan
发明人： Harry John Wadsworth , Bo Shan , Dennis O'Shea , Joanna Marie Passmore , William John Trigg , Amanda Ewan
IPC分类号： A61K51/00 , A61K36/14
CPC分类号： C07D209/94 , A61K51/0446 , A61K51/0455 , A61K51/0468 , C07B59/002 , C07B2200/05 , C07D209/88 , C07D295/192 , C07D401/06 , C07D495/04
摘要： An indole-based in vivo imaging agent is provided by the present invention that binds with high affinity to PBR, has good uptake into the brain following administration, and which has good selective binding to PBR. The invention also includes a precursor compound useful in the synthesis of the in vivo imaging agent of the invention, as well as a method for synthesis of said in vivo imaging agent comprising use of said precursor compound, and a kit for carrying out said method. Also provided is a cassette for automated synthesis of the in vivo imaging agent. Further aspects of the invention include a radiopharmaceutical composition comprising the in vivo imaging agent of the invention, and methods for the use of said in vivo imaging agent.
摘要翻译：通过本发明提供的以吲哚为基础的体内显像剂以高亲和力结合PBR，在给药后具有良好的摄入脑中，并具有良好的选择性结合PBR。本发明还包括可用于合成本发明的体内显像剂的前体化合物，以及包含使用所述前体化合物的所述体内显像剂的合成方法和用于实施所述方法的试剂盒。还提供了用于体内成像剂的自动合成的盒。本发明的其它方面包括包含本发明的体内显像剂的放射性药物组合物和使用所述体内显像剂的方法。

2. 发明授权

US08771641B2 Aryloxyanilide imaging agents 失效
标题翻译：芳氧基苯胺显像剂
公开(公告)号：US08771641B2
公开(公告)日：2014-07-08
申请号：US13510041
申请日：2010-12-16
申请人： Harry John Wadsworth , Dennis O'Shea
发明人： Harry John Wadsworth , Dennis O'Shea
IPC分类号： A61K51/04 , A61K31/44
CPC分类号： A61K51/0423 , A61K51/0419 , A61K51/0425 , B01L3/52 , C07D307/79 , C07D307/81 , C07D317/46 , C07D317/58 , C07D319/18 , C07D321/10
摘要： The present invention provides a novel radiolabeled aryloxyalinine derivative suitable for in vivo imaging. In comparison to known aryloxyalinine derivative in vivo imaging agents, the in vivo imaging agent of the present invention has better properties for in vivo imaging. The in vivo imaging agent of the present invention demonstrates good selective binding to the peripheral benzodiazepine receptor (PBR), in combination with good brain uptake and in vivo kinetics following administration to a subject.
摘要翻译：本发明提供适用于体内成像的新型放射性标记的芳氧基亚胺衍生物。与已知的芳氧基亚胺衍生物体内显像剂相比，本发明的体内显像剂具有更好的体内成像性能。本发明的体内显像剂与外用苯并二氮杂受体（PBR）具有良好的选择性结合，结合良好的脑摄取和给予受试者后的体内动力学。

3. 发明申请

US20120020884A1 INDOLE DERIVATIVES 有权
标题翻译： INDOLE DORIVATIVES
公开(公告)号：US20120020884A1
公开(公告)日：2012-01-26
申请号：US13258465
申请日：2010-03-26
申请人： Harry John Wadsworth , Bo Shan , Dennis O'shea , Joanna Marie Passmore , William John Trigg , Amanda Ewan
发明人： Harry John Wadsworth , Bo Shan , Dennis O'shea , Joanna Marie Passmore , William John Trigg , Amanda Ewan
IPC分类号： A61K51/04 , B01J19/00 , C07D401/08 , C07D495/04 , C07D209/94 , C07D209/80
CPC分类号： C07D209/94 , A61K51/0446 , A61K51/0455 , A61K51/0468 , C07B59/002 , C07B2200/05 , C07D209/88 , C07D295/192 , C07D401/06 , C07D495/04
摘要： An indole-based in vivo imaging agent is provided by the present invention that binds with high affinity to PBR, has good uptake into the brain following administration, and which has good selective binding to PBR. The invention also includes a precursor compound useful in the synthesis of the in vivo imaging agent of the invention, as well as a method for synthesis of said in vivo imaging agent comprising use of said precursor compound, and a kit for carrying out said method. Also provided is a cassette for automated synthesis of the in vivo imaging agent. Further aspects of the invention include a radiopharmaceutical composition comprising the in vivo imaging agent of the invention, and methods for the use of said in vivo imaging agent.
摘要翻译：通过本发明提供的以吲哚为基础的体内显像剂以高亲和力结合PBR，在给药后具有良好的摄入脑中，并具有良好的选择性结合PBR。本发明还包括可用于合成本发明的体内显像剂的前体化合物，以及包含使用所述前体化合物的所述体内显像剂的合成方法和用于实施所述方法的试剂盒。还提供了用于体内成像剂的自动合成的盒。本发明的其它方面包括包含本发明的体内显像剂的放射性药物组合物和使用所述体内显像剂的方法。

4. 发明申请

US20110110865A1 CHELATROS, PARAMAGNETIC CHELATES THEREOF AND THEIR USE AS CONTRAST AGENTS IN MAGNETIC RESONANCE IMAGING (MRI) 失效
标题翻译： CHELATROS，其参考文献及其作为对比剂在磁共振成像（MRI）中的使用
公开(公告)号：US20110110865A1
公开(公告)日：2011-05-12
申请号：US12672113
申请日：2008-08-12
申请人： Oskar Axelsson , Horry John Wadsworth , Ian Martin Newington , Dennis O'Shea
发明人： Oskar Axelsson , Horry John Wadsworth , Ian Martin Newington , Dennis O'Shea
IPC分类号： A61K49/06 , C07D407/14 , C07D401/14 , C07F15/00 , C08G69/48 , A61B5/055
CPC分类号： C07D401/14 , C07D213/81 , C07D309/40 , C07D407/14
摘要： The present invention relates to chelators, in particular to chelators which are capable of forming complexes, i.e. paramagnetic chelates, with paramagnetic metal ions. The invention also relates to said paramagnetic chelates, said paramagnetic chelates linked to other molecules and their use as contrast agents in magnetic resonance imaging (MRI).
摘要翻译：本发明涉及螯合剂，特别涉及能够与顺磁金属离子形成络合物即顺磁性螯合物的螯合剂。本发明还涉及所述顺磁性螯合物，所述顺磁性螯合物与其它分子连接，以及它们在磁共振成像（MRI）中作为造影剂的用途。

5. 发明授权

US09481685B2 Imaging neuroinflammation 有权
标题翻译：成像神经炎症
公开(公告)号：US09481685B2
公开(公告)日：2016-11-01
申请号：US13119450
申请日：2009-10-02
申请人： Harry John Wadsworth , Bo Shan , Dennis O'Shea , Joanna Marie Passmore , William John Trigg
发明人： Harry John Wadsworth , Bo Shan , Dennis O'Shea , Joanna Marie Passmore , William John Trigg
IPC分类号： A61K51/00 , A61M36/14 , C07D495/04 , A61K51/04
CPC分类号： C07D495/04 , A61K51/0446
摘要： The present invention concerns in vivo imaging and in particular in vivo imaging of the peripheral benzodiazepine receptor (PBR). A tetracyclic indole in vivo imaging agent is provided that binds with high affinity to PBR, has good uptake into the brain following administration, and which preferentially binds to tissues expressing higher levels of PBR. The present invention also provides a precursor compound useful in the synthesis of the in vivo imaging agent of the invention, as well as a method for synthesis of said in vivo imaging agent comprising use of said precursor compound, and a kit for carrying out said method. A cassette for the automated synthesis of the in vivo imaging agent is also provided. In addition, the invention provides a radiopharmaceutical composition comprising the in vivo imaging agent of the invention, as well as methods for the use of said in vivo imaging agent.
摘要翻译：本发明涉及体内成像，特别是周边苯二氮卓受体（PBR）的体内成像。提供四环吲哚体内显像剂，其以高亲和力与PBR结合，在给药后具有良好的摄入脑中，并优先结合表达较高水平的PBR的组织。本发明还提供了可用于合成本发明的体内显像剂的前体化合物，以及包含使用所述前体化合物的所述体内显像剂的合成方法和用于实施所述方法的试剂盒。还提供了用于体内成像剂的自动合成的盒。此外，本发明提供了包含本发明的体内显像剂的放射性药物组合物，以及使用所述体内显像剂的方法。

6. 发明授权

US08501153B2 Active enantiomer 有权
标题翻译：活性对映异构体
公开(公告)号：US08501153B2
公开(公告)日：2013-08-06
申请号：US12880218
申请日：2010-09-13
申请人： Radha Achanath , Srinath Balaji , Afsal M. Kadavilpparampu Mohamed , Umamaheshwar Mokkapati , Steven Fairway , Dimitrios Mantzilas , Dennis O'Shea , William John Trigg , Harry John Wadsworth , Joanna Marie Passmore , Bo Shan
发明人： Radha Achanath , Srinath Balaji , Afsal M. Kadavilpparampu Mohamed , Umamaheshwar Mokkapati , Steven Fairway , Dimitrios Mantzilas , Dennis O'Shea , William John Trigg , Harry John Wadsworth , Joanna Marie Passmore , Bo Shan
IPC分类号： A61K51/00 , A61K36/14
CPC分类号： C07D209/94 , A61K51/0446 , A61K51/0455 , A61K51/0468 , C07B59/002 , C07B2200/05 , C07D209/88 , C07D295/192 , C07D401/06 , C07D495/04
摘要： The present invention provides a PET tracer that has improved properties for imaging the peripheral benzodiazepine receptor (PBR) as compared with known such PET tracers. The present invention also provides a precursor compound useful in the preparation of the PET tracer of the invention and methods for the preparation of said precursor compound and said PET tracer. Also provided by the present invention is a radiopharmaceutical composition comprising the PET tracer of the invention. Methods for using the PET tracer and the radiopharmaceutical composition are also provided.
摘要翻译：本发明提供了与已知的这种PET示踪剂相比具有改进的外周苯并二氮杂受体（PBR）成像的特性的PET示踪剂。本发明还提供了可用于制备本发明的PET示踪剂的前体化合物和用于制备所述前体化合物和所述PET示踪剂的方法。本发明还提供了包含本发明的PET示踪剂的放射性药物组合物。还提供了使用PET示踪剂和放射性药物组合物的方法。

7. 发明授权

US08475768B2 Paramagnetic chelates thereof and their use as contrast agents in magnetic resonance imaging (MRI) 失效
标题翻译：其磁性螯合物及其作为造影剂用于磁共振成像（MRI）
公开(公告)号：US08475768B2
公开(公告)日：2013-07-02
申请号：US12672113
申请日：2008-08-12
申请人： Oskar Axelsson , Harry John Wadsworth , Ian Martin Newington , Dennis O'Shea
发明人： Oskar Axelsson , Harry John Wadsworth , Ian Martin Newington , Dennis O'Shea
IPC分类号： A61B5/055 , C08G18/62 , C07D213/62
CPC分类号： C07D401/14 , C07D213/81 , C07D309/40 , C07D407/14
摘要： The present invention relates to chelators, in particular to chelators which are capable of forming complexes, i.e. paramagnetic chelates, with paramagnetic metal ions. The invention also relates to said paramagnetic chelates, said paramagnetic chelates linked to other molecules and their use as contrast agents in magnetic resonance imaging (MRI).
摘要翻译：本发明涉及螯合剂，特别涉及能够与顺磁金属离子形成络合物即顺磁性螯合物的螯合剂。本发明还涉及所述顺磁性螯合物，所述顺磁性螯合物与其它分子连接，以及它们在磁共振成像（MRI）中作为造影剂的用途。

8. 发明申请

US20110070161A1 ACTIVE ENANTIOMER 有权
标题翻译：活跃的ENANTIOMER
公开(公告)号：US20110070161A1
公开(公告)日：2011-03-24
申请号：US12880218
申请日：2010-09-13
申请人： RADHA ACHANATH , SRINATH BALAJI , STEVEN FAIRWAY , AFSAL M. KADAVILPPARAMPU MOHAMED , DIMITRIOS MANTZILAS , UMAMAHESHWAR MOKKAPATI , DENNIS O'SHEA , JOANNA MARIE PASSMORE , BO SHAN , WILLIAM JOHN TRIGG , HARRY JOHN WADSWORTH
发明人： RADHA ACHANATH , SRINATH BALAJI , STEVEN FAIRWAY , AFSAL M. KADAVILPPARAMPU MOHAMED , DIMITRIOS MANTZILAS , UMAMAHESHWAR MOKKAPATI , DENNIS O'SHEA , JOANNA MARIE PASSMORE , BO SHAN , WILLIAM JOHN TRIGG , HARRY JOHN WADSWORTH
IPC分类号： A61K51/04 , C07D209/88 , B01J19/00
CPC分类号： C07D209/94 , A61K51/0446 , A61K51/0455 , A61K51/0468 , C07B59/002 , C07B2200/05 , C07D209/88 , C07D295/192 , C07D401/06 , C07D495/04
摘要： The present invention provides a PET tracer that has improved properties for imaging the peripheral benzodiazepine receptor (PBR) as compared with known such PET tracers. The present invention also provides a precursor compound useful in the preparation of the PET tracer of the invention and methods for the preparation of said precursor compound and said PET tracer. Also provided by the present invention is a radiopharmaceutical composition comprising the PET tracer of the invention. Methods for using the PET tracer and the radiopharmaceutical composition are also provided.
摘要翻译：本发明提供了与已知的这种PET示踪剂相比具有改进的外周苯并二氮杂受体（PBR）成像的特性的PET示踪剂。本发明还提供了可用于制备本发明的PET示踪剂的前体化合物和用于制备所述前体化合物和所述PET示踪剂的方法。本发明还提供了包含本发明的PET示踪剂的放射性药物组合物。还提供了使用PET示踪剂和放射性药物组合物的方法。

9. 发明授权

US08158804B2 Chelating agents 失效
标题翻译：螯合剂
公开(公告)号：US08158804B2
公开(公告)日：2012-04-17
申请号：US12521195
申请日：2008-01-11
申请人： Harry John Wadsworth , Ian Martin Newington , Clare L. Jones , Amanda Ewan , Dennis O'Shea
发明人： Harry John Wadsworth , Ian Martin Newington , Clare L. Jones , Amanda Ewan , Dennis O'Shea
IPC分类号： C07D213/89 , C07D213/69
CPC分类号： C07D213/81 , A61K49/103
摘要： The present invention relates to chelating agents, in particular to chelating agents which are capable of forming complexes with paramagnetic metal ions such as iron (III) and gadolinium (III). The invention also relates to the complexes formed and their use as MRI contrast agents.
摘要翻译：本发明涉及螯合剂，特别涉及能够与顺磁金属离子如铁（III）和钆（III）形成络合物的螯合剂。本发明还涉及形成的复合物及其作为MRI造影剂的用途。

10. 发明申请

US20100008864A1 AROMATIC MULTIMERS 审中-公开
公开(公告)号：US20100008864A1
公开(公告)日：2010-01-14
申请号：US12499281
申请日：2009-07-08
申请人： Andreas Meijer , Harry John Wadsworth , Ian Martin Newington , Clare L. Jones , Amanda Ewan , Dennis O'Shea , Oskar Axelsson , Anders Brathe , Andreas Olsson , John Henrik Johansen , Duncan George Wynn
发明人： Andreas Meijer , Harry John Wadsworth , Ian Martin Newington , Clare L. Jones , Amanda Ewan , Dennis O'Shea , Oskar Axelsson , Anders Brathe , Andreas Olsson , John Henrik Johansen , Duncan George Wynn
IPC分类号： A61K49/10 , C07F15/00
CPC分类号： A61K49/124
摘要： The present invention relates to novel compounds of formula (I) and (II), compositions comprising compounds of formula (II) and their use as contrast agents in magnetic resonance (MR) imaging (MRI) and MR spectroscopy (MRS).
摘要翻译：本发明涉及式（I）和（II）的新化合物，包含式（II）化合物的组合物及其作为磁共振（MR）成像（MRI）和MR光谱学（MRS）中的造影剂的用途。

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